Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists

Gregory J Pacofsky; Jeffrey A Stafford; Richard F Cox; Jill R Cowan; George F Dorsey Jr; Stephen S Gonzales; Istvan Kaldor; George W Koszalka; George G Lovell; Maggie S McIntyre; Jeffrey H Tidwell; Dan Todd; Graham Whitesell; Robert P Wiard; Paul L Feldman

doi:10.1016/s0960-894x(02)00513-9

Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3219-22. doi: 10.1016/s0960-894x(02)00513-9.

Authors

Gregory J Pacofsky¹, Jeffrey A Stafford, Richard F Cox, Jill R Cowan, George F Dorsey Jr, Stephen S Gonzales, Istvan Kaldor, George W Koszalka, George G Lovell, Maggie S McIntyre, Jeffrey H Tidwell, Dan Todd, Graham Whitesell, Robert P Wiard, Paul L Feldman

Affiliation

¹ GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.

PMID: 12372538
DOI: 10.1016/s0960-894x(02)00513-9

Abstract

The ultrashort-acting benzodiazepine (USA BZD) agonists reported previously have been structurally modified to improve aqueous solubility. Lactam-to-amidine modifications, replacement of the C5-haloaryl ring, and annulation of heterocycles are presented. These analogues retain BZD receptor potency and full agonism profiles.

MeSH terms

Animals
Benzodiazepines / chemical synthesis*
Benzodiazepines / pharmacokinetics
Benzodiazepines / pharmacology*
Drug Design
GABA-A Receptor Agonists*
Indicators and Reagents
Molecular Conformation
Postural Balance / drug effects
Rats
Solubility
Structure-Activity Relationship

Substances

GABA-A Receptor Agonists
Indicators and Reagents
Benzodiazepines